Discovery of Potent and Selective Benzothiazole Hydrazone Inhibitors of Bcl-X-L

Brad E Sleebs; Wilhemus JA Kersten; Sanji Kulasegaram; George Nikolakopoulos; Effie Hatzis; Rebecca M Moss; John P Parisot; Hong Yang; Peter E Czabotar; W Douglas Fairlie; Erinna F Lee; Jerry M Adams; Lin Chen; Mark F van Delft; Kym N Lowes; Andrew Wei; David CS Huang; Peter M Colman; Ian P Street; Jonathan B Baell; Keith Watson; Guillaume Lessene

Journal article

Discovery of Potent and Selective Benzothiazole Hydrazone Inhibitors of Bcl-X-L

Brad E Sleebs, Wilhemus JA Kersten, Sanji Kulasegaram, George Nikolakopoulos, Effie Hatzis, Rebecca M Moss, John P Parisot, Hong Yang, Peter E Czabotar, W Douglas Fairlie, Erinna F Lee, Jerry M Adams, Lin Chen, Mark F van Delft, Kym N Lowes, Andrew Wei, David CS Huang, Peter M Colman, Ian P Street, Jonathan B Baell Show all

Journal of Medicinal Chemistry | AMER CHEMICAL SOC | Published : 2013

DOI: 10.1021/jm400556w

University of Melbourne Researchers

Peter Czabotar Author Medical Biology (W.E.H.I.)

Ian Street Author Medical Biology (W.E.H.I.)

Guillaume Lessene Author Medical Biology (W.E.H.I.)

Kym Lowes Author Medical Biology (W.E.H.I.)

Jerry Adams Author Medical Biology (W.E.H.I.)

Grants

Awarded by National Health and Medical Research Council (NHMRC)

Awarded by Leukemia and Lymphoma Society

Awarded by Cancer Council of Victoria

Awarded by NHMRC

Funding Acknowledgements

We thank Steve Elmore and Abbvie for providing 1. We also thank our colleagues at the Hall Institute for their work on the Bcl-2 family of proteins that has led to this contribution and for discussions during this work. In particular: Andreas Strasser and Suzanne Cory. This work was supported by fellowships and grants from the Australian Research Council (fellowship to P.E.C.), the National Health and Medical Research Council (NHMRC, fellowships to J.M.A, J.B.B., P.M.C. and D.C.S.H.; development grant 305536 and program grants 257502, 461221 and 1016701), the Leukemia and Lymphoma Society (specialized center of research grant nos. 7015 and 7413), the Cancer Council of Victoria (fellowship to P.M.C.; grant-in-aid 461239) and the Australian Cancer Research Foundation. Infrastructure support from the NHMRC Independent Research Institutes Infrastructure Support Scheme grant no. 361646 and a Victorian State Government OIS grant are gratefully acknowledged.